HMTase Inhibitor V, UNC0224 (Histone Lysine Methyltransferase Inhibitor V, UNC0224, 7-(3-Dimethylaminopropoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine, H2O)

Blue Ice

503, 7

Supplied as a liquid in DMSO.

A quinazolinamine compound that acts as a potent, reversible and SAM (S-adenosylmethionine) non-competitive inhibitor of methyltransferases G9a (H3K9 HMT/EHMT2; IC50=15nM; =23nM) and GLP (G9a-like protein/EHMT1; IC50=20nM). Displays 1, 000-fold greater selectivity for G9a over SET7/9 (H3K4 HMTase), SET8/PreSET7 (H4K20 HMTase), PRMT3 (MTase) and JMJD2E (demethylase), and minimally affects the activities of a broad range of GPCRs, ion-channels and transporters in a 30-target selectivity panel, with the exception of muscarinic M2 receptor and histamine H1 receptors (82% and 31% inhibition at 1uM, respectively).

CAS Number:
1197196-48-7

Formula:
C₂₆H₄₃N₇O₂ • H₂O

Molecular Weight:
503.7

Storage and Stability:
May be stored at 4°C for short-term only. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.